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Entecavir monohydrate (BMS-200475) is a selective inhibitor of the replication of the hepatitis B virus (HBV). It, a new deoxyguanine nucleoside analog.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $30 | In Stock | In Stock | |
| 5 mg | $44 | In Stock | In Stock | |
| 10 mg | $77 | In Stock | In Stock | |
| 25 mg | $116 | In Stock | In Stock | |
| 50 mg | $162 | In Stock | In Stock | |
| 100 mg | $243 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $48 | In Stock | In Stock |
| Description | Entecavir monohydrate (BMS-200475) is a selective inhibitor of the replication of the hepatitis B virus (HBV). It, a new deoxyguanine nucleoside analog. |
| Targets&IC50 | HBV (HepG2 cells):3.75 nM(ec50) |
| In vitro | In ducks, Entecavir administration results in a 4-log reduction of serum DHBV DNA levels within 80 days and a 2- to 3-log decrease in hepatitis B virus surface antigen within 120 days. Treatment with Entecavir also decreases replication intermediates of DHBV DNA in the liver by a factor of 70, while covalently closed circular DNA levels are only reduced fourfold under stable template conditions. Additionally, Entecavir reduces both the intensity of antigen staining and the percentage of antigen-positive cells in the liver, although there is an increase in antigen staining intensity in bile duct cells. |
| In vivo | In liver biopsy samples, Entecavir reduces both covalently closed circular DNA and the negativity of the hepatitis B virus core antigen. Entecavir triphosphate acts as an effective inhibitor of the wild-type HBV polymerase and is 100-300 times more potent than lamivudine triphosphate against 3TC-resistant HBV polymerase. To inhibit the replication of 3TC-resistant HBV, Entecavir requires a concentration that is 20-30 times higher. With an EC50 of 0.1 nM, Entecavir demonstrates significant activity against HIV. It can be utilized in a single-cycle, single-cell line pseudovirus assay, measuring green fluorescent protein in CD4+ lymphocytes using fluorescence-activated cell sorting. |
| Cell Research | BMS 200475 is prepared in phosphate-buffered saline (PBS) and diluted with appropriate medium containing 2% fetal bovine serum. HepG2 2.2.15 cells are plated at a density of 5×105 cells per well on 12-well Biocoat collagen-coated plates and are maintained in a confluent state for 2 to 3 days before being overlaid with 1 mL of medium spiked with BMS 200475. Quantification of HBV was performed on day 10[1]. |
| Synonyms | SQ 34676, Entecavir hydrate, BMS-200475 |
| Molecular Weight | 295.3 |
| Formula | C12H15N5O3·H2O |
| Cas No. | 209216-23-9 |
| Smiles | O.Nc1nc(=O)c2ncn([C@H]3C[C@H](O)[C@@H](CO)C3=C)c2[nH]1 |
| Relative Density. | 1.81 |
| Storage | keep away from direct sunlight,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 55 mg/mL (186.25 mM), Sonication is recommended. Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.5 mg/mL (8.47 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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